Journal of the Korea Academia-Industrial cooperation Society (한국산학기술학회논문지)

The Korea Academia-Industrial cooperation Society (한국산학기술학회)
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Preparation and Dissolution Properties of Oral Controlled Release Formulation Containing Carvedilol

카르베딜롤을 함유하는 경구제어 방출형 제제의 제조 및 용출특성

  • Choi, Won-Sik (Department of Biotechnology, Soonchunhyang University) ;
  • Kim, Yong-Nam (Department of Biotechnology, Soonchunhyang University) ;
  • Nam, Seok-Woo (Department of Biotechnology, Soonchunhyang University) ;
  • Yang, Jin-Ah (Department of Biotechnology, Soonchunhyang University)
  • 최원식 (순천향대학교 유전공학과) ;
  • 김용남 (순천향대학교 유전공학과) ;
  • 남석우 (순천향대학교 유전공학과) ;
  • 양진아 (순천향대학교 유전공학과)
  • Received : 2010.04.22
  • Accepted : 2010.07.06
  • Published : 2010.07.31
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Abstract

We prepared sustained release matrix system which contains carvedilol with Compritol 888 ATO used as lipophilic sustained release excipient and hydroxypropyl methyl cellulose (HPMC) or polyethylene oxide (PEO) used as hydrophilic sustained release polymer. Wet granulation compressed method was used for preparing carvedilol sustained release matrix tablets. When carvedilol sustained release matrix tablets were prepared, we evaluated the drug release kinetics which is affected by Compritol 888 ATO ratio, a kind of hydrophilic polymer (HPMC, PEO) and hot melt coating coagglutination (HMCC) process was done. The drug release kinetics was measured for 24 hours in pH 1.2 simulated gastric fluid and pH 6.8 simulated intestinal fluid, using a dissolution tester at $37.5^{\circ}C$ in 50 rpm. Dissolution rate of controlled release matrix tablets of carvedilol was evaluated by paddle method. We confirmed that HMCC process was very effective to controlled release of drugs. The rate of Compritol 888 ATO, as a lipidic material, can control the drug release pattern about the elution rate of 95% and 24 hours delay than that of the normal tablet.

고혈압 치료제인 카르베딜롤을 모델약물로 하여 새로운 서방성 방출 제어형 매트릭스 정제를 제조하기 위하여 소수성 서방성 부형제인 Compritol 888 ATO와 친수성 고분자인 hydroxypropyl methyl cellulose (HPMC) 또는 polyethylene oxide (PEO)를 이용하여 방출 제어형 매트릭스 정제를 제조하였다. 카르베딜롤 방출 제어형 매트릭스 정제의 제조 시 Compritol 888 ATO의 비율과 친수성 고분자의 종류 및 비율, hot melt coating coagglutination (HMCC) rocess의 적용 유무에 따른 카르베딜롤의 방출 양상을 위하여 용출시험기를 사용하여 pH 1.2의 인공위액과 pH 6.8의 인공장액에서 24시간 동안 $37^{\circ}C$, 50 rpm으로 용출시험을 실시하였다. 그 결과, HMCC process를 적용한 모든 제제가 약물의 방출 제어에 매우 효과적인 것을 확인하였다. 또한 소수성 서방성 부형제인 Compritol 888 ATO의 비율에 따라 약물의 방출 양상 및 시간이 기존 일반정제에 비하여 약 95%의 용출률을 나타내었으며 24시간까지 지연됨을 확인할 수 있었다.

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